| 摘要 |
Disclosed herein are phosphorothioate nucleotide analogs, such as thiophosphoramidate prodrugs and thiohosphates (including α-thiomonophosphates, α-thiodiphosphates, and α-thiotriphosphates), methods of synthesizing phosphorothioate nucleotide analogs, such as thiophosphoramidate prodrugs and thiophosphates, and methods of treating viral infections such as HCV, with the phosphorothioate nucleotide analogs, such as thiophosphoramidate prodrugs and thiophosphates. |
| 主权项 |
1. A compound of Formula (I) or a pharmaceutically acceptable salt thereof: wherein: B1 is an optionally substituted pyrimidine base; R1 is an optionally substituted N-linked α-amino acid or an optionally substituted N-linked α-amino acid ester derivative; R2 is selected from the group consisting of an optionally substituted aryl and an optionally substituted monocyclic heteroaryl; R3a and R3b are both hydrogen; R4 is hydrogen; R5 is hydrogen; R6 is selected from the group consisting of hydrogen, —OR12 and —OC(═O)R13; R7 is selected from the group consisting of hydrogen, —OR14 and —OC(═O)R15;
or R6 and R7 are both oxygen atoms and linked together by a carbonyl group; R8 is selected from the group consisting of azido, cyano, halogen, and unsubstituted C1-C6 alkyl; R9 is hydrogen; R12 and R14 are selected from the group consisting of hydrogen or an unsubstituted C1-6 alkyl; R13 and R15 are selected from the group consisting of an unsubstituted C1-6 alkyl or an unsubstituted C3-6 cycloalkyl; and wherein when a substituent is substituted, the substituent is substituted with a group individually and independently selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl, cycloalkenyl, C6-C10 aryl, 4 to 14 atom heteroaryl, 3 to 18 atom heteroalicyclyl, (aryl)C1-4 alkyl, (heteroaryl)C1-4 alkyl, (heteroalicyclyl) C1-4 alkyl, hydroxy, alkoxy, aryloxy, acyl, cyano, halogen, O-carbamyl, N-carbamyl, N-thiocarbamyl, C-amido, N-amido, S-sulfonamido, N-sulfonamido, C-carboxy, O-carboxy, nitro, sulfonyl, haloalkyl, haloalkoxy, an amino, a mono-substituted amino group and a di-substituted amino group. |
